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Chemical Structure : CVN424
CAS No.: 2254706-21-1
Catalog No.: PC-72762Not For Human Use, Lab Use Only.
CVN424 (CVN 424) is a highly potent, selective, brain-penetrant, orally active GPR6 inverse agonist with EC50 of 38 nM.
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CVN424 (CVN 424) is a highly potent, selective, brain-penetrant, orally active GPR6 inverse agonist with EC50 of 38 nM.
Oral administration of CVN424 dose-dependently increases locomotor activity and reverses haloperidol-induced catalepsy.
CVN424 restored mobility in bilateral 6-hydroxydopamine lesion model of Parkinson disease.
CVN424 is brain-penetrant and shows dose-dependent receptor occupancy that attained brain 50% of receptor occupancy at plasma concentrations of 6.0 and 7.4 ng/ml in mice and rats, respectively.
CVN424 is effective in preclinical models and is a potential therapeutic for improving motor function in patients with Parkinson disease.
| M.Wt | 473.525 | |
| Formula | C24H29F2N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-1-(2-(4-(2,4-difluorophenoxy)piperidin-1-yl)-3-((tetrahydrofuran-3-yl)amino)-7,8-dihydropyrido[3,4-b]pyrazin-6(5H)-yl)ethan-1-one |
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1. Brice NL, et al. J Pharmacol Exp Ther. 2021 Jun;377(3):407-416.
2. M, Green J, et al. J Med Chem. 2021 Jul 22;64(14):9875-9890.
3. Margolin DH, et al. J Pharmacol Exp Ther. 2022 Feb 2:JPET-AR-2021-000842.
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